| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Calcium-sensing receptor (CaSR). Calcium-Sensing Receptor Antagonists I functions as an antagonist to the parathyroid hormone receptors that sense calcium.
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|---|---|
| ln Vitro |
Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors. It is useful for osteoporosis and other bone conditions. IC50 value: Target: CaSR.
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| ln Vivo |
No specific in vivo activity data is available for Calcium-Sensing Receptor Antagonists I. It is useful for osteoporosis and other bone conditions, suggesting potential for in vivo studies in bone disease models.
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| Enzyme Assay |
In vitro receptor binding assays for Calcium-Sensing Receptor Antagonists I involve measuring its affinity for the calcium-sensing receptor (CaSR) using radioligand displacement or functional assays (e.g., calcium mobilization). IC50 values are determined from dose-response curves.
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| Cell Assay |
The in vitro cellular activity of Calcium-Sensing Receptor Antagonists I is evaluated in cells expressing the CaSR. Cells are treated with the compound, and receptor-mediated signaling (e.g., intracellular calcium changes, ERK phosphorylation) is measured. The compound's antagonist activity is assessed by its ability to block CaSR activation by calcium or other agonists.
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| Animal Protocol |
No specific in vivo animal experimental protocols are available for Calcium-Sensing Receptor Antagonists I. For studying CaSR antagonism in bone disease models, the compound would typically be administered via intraperitoneal injection or oral gavage in rodent models of osteoporosis or hyperparathyroidism. Endpoints would include bone mineral density, serum calcium and PTH levels.
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| ADME/Pharmacokinetics |
Calcium-Sensing Receptor Antagonists I has a molecular formula of C23H24N2O2 and a molecular weight of 360.45. Solubility: DMSO: 100 mg/mL (277.43 mM). Storage: powder at -20degC for 3 years. In vivo formulation: 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline.
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| Toxicity/Toxicokinetics |
No specific toxicological data is available for Calcium-Sensing Receptor Antagonists I. As a research compound intended for laboratory use, standard safety precautions should be observed. No clinical toxicity studies have been reported.
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| References | |
| Additional Infomation |
Calcium-Sensing Receptor Antagonists I is an antagonist of the calcium-sensing receptor (CaSR) useful for osteoporosis and other bone conditions. It is a click chemistry reagent containing an Alkyne group. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C23H24N2O2
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|---|---|
| Molecular Weight |
360.44886
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| Exact Mass |
360.184
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| CAS # |
478963-79-0
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| PubChem CID |
10109178
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.085g/cm3
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| Boiling Point |
510.1ºC at 760 mmHg
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| Flash Point |
262.299ºC
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| Index of Refraction |
1.572
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| LogP |
4.779
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
607
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RXVZJHDMMKTKDR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24N2O2/c1-6-13-27-19-11-12-21-20(14-19)22(24-23(26)25(21)16(4)5)18-9-7-17(8-10-18)15(2)3/h1,7-12,14-16H,13H2,2-5H3
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| Chemical Name |
1-propan-2-yl-4-(4-propan-2-ylphenyl)-6-prop-2-ynoxyquinazolin-2-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~277.43 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (9.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3.25 mg/mL (9.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7743 mL | 13.8715 mL | 27.7431 mL | |
| 5 mM | 0.5549 mL | 2.7743 mL | 5.5486 mL | |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7743 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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